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基于改性多糖的黏膜黏附混合聚合物/脂质体糊剂。

Mucoadhesive Hybrid Polymer/Liposome Pastes Based on Modified Polysaccharides.

机构信息

The Inter-Departmental Program of Biotechnology, Technion - Israel Institute of Technology, Haifa 3200003, Israel.

Department of Chemical Engineering, Technion - Israel Institute of Technology, Haifa 3200003, Israel.

出版信息

J Pharm Sci. 2019 Dec;108(12):3814-3822. doi: 10.1016/j.xphs.2019.08.022. Epub 2019 Sep 3.

DOI:10.1016/j.xphs.2019.08.022
PMID:31491439
Abstract

Mucoadhesive hybrid polymer/liposome paste is a new drug delivery system presenting controllable and tailorable delivery mechanism. By using mucoadhesive material, the delivery can be more specific and local. Here, we present a study investigating the effect of polymer type, concentration, functional end group, and cross-linking on the release profile of nanoliposomes from polymer pastes. Polymer pastes can be expected to combine the mucoadhesion mechanisms of dry and wet dosage forms but have not been studied extensively. To better understand the mucoadhesion of pastes, we investigated a series of pastes based on the same polymer and used different chemical modifications that can produce interactions at different levels. Native and thiolated polymers presented enhanced mucoadhesion in a wet environment in comparison to acrylated polymers which dissolved rapidly because of the enhanced solubility of PEG chains in water. Paste cross-linking resulted in a sustained release profile compared to non-cross-linked pastes. Pectin-SH pastes, especially 3% (w/v), showed a linear liposomal release profile which is ascribed to the combination of ionic cross-linking and disulfide bridging. By configuring the polymer type or concentration, we can control the release mechanisms and achieve distinct inherent properties which can be applied for diverse medical applications.

摘要

粘弹性聚合物/脂质体糊剂是一种新的药物传递系统,具有可控和可定制的传递机制。通过使用粘弹性材料,传递可以更加具体和局部。在这里,我们研究了聚合物类型、浓度、官能团末端和交联对纳米脂质体从聚合物糊剂中释放的影响。聚合物糊剂有望结合干和湿剂型的粘弹性机制,但尚未得到广泛研究。为了更好地理解糊剂的粘弹性,我们研究了一系列基于相同聚合物的糊剂,并使用了不同的化学修饰,这些修饰可以在不同的水平上产生相互作用。与丙烯酰化聚合物相比,天然和巯基化聚合物在湿环境中表现出增强的粘弹性,因为 PEG 链在水中的溶解度增强。与非交联糊剂相比,糊剂交联导致释放曲线持续。果胶-SH 糊剂,特别是 3%(w/v),显示出线性脂质体释放曲线,这归因于离子交联和二硫键桥接的结合。通过配置聚合物类型或浓度,我们可以控制释放机制并获得独特的固有特性,可应用于各种医疗应用。

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